Abstract The straightforward laboratory preparation of structural motifs commonly found in therapeutic agents is a major driving force in catalysis-based reaction design. In our laboratory we have adopted cooperative catalysis, an approach that emulates mechanisms encountered in enzymatic activity. In such a regime, merges of two (or more) simultaneous and complementary catalysis events are merged to forge a single chemical bond, via hitherto inaccessible chemical reactivity. Despite the infancy of this area, it promises much for the design of new, efficient and operationally trivial catalytic asymmetric reactions, and expedite the design, development and manufacture of medicines to manage and treat diseases. Based on exciting preliminary data we have obtained in the arena of cooperative catalysis, the program detailed in this proposal will provide the scientific community with straightforward, reliable and flexible methods for chemical synthesis This work will significantly impact human health and medicine by establishing routine synthetic protocols for the preparation of valuable molecular scaffolds, which will contribute to the design and development of new clinical agents.